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Purpose The metabolism and disposition of the first-in-class DOT1L inhibitor, EPZ-5676 (pinometostat), was investigated in rat and dog. Metabolite profiles were compared with those from adult patients in the first-in-man phase 1 study as well as the cross-species metabolism observed in vitro. Methods EPZ-5676 was administered to rat and dog as a 24-h IV infusion of [14C]-EPZ-5676 for determination...
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